▎ 摘　　要

NOVELTY - Constructing C(sp3)-C(sp2) bond, comprises directly coupling the amino acid beta-C(sp3) and ring carbon C(sp2) where phenolic hydroxy group is located to construct carbon-carbon bond. USE - The C(sp3)-C(sp2) bond is useful for preparing various unnatural beta-aryl amino acids (claimed). ADVANTAGE - The method has simple operation, low cost, strong reaction versatility, and high yield and stereoselectivity. DETAILED DESCRIPTION - An INDEPENDENT CLAIM is also included for preparing beta-aryl amino acids of formula (V) comprising dissolving purified amino acid beta-arylation product (II) in 0.5-2 N mineral acid aqueous solution, and hydrolyzing under the assistance of 25 W microwave, then it is neutralizing with aqueous sodium hydroxide solution, extracting with ethyl acetate to recover the ligand L1, concentrating aqueous phase, and recrystallizing residue to obtain beta-aryl amino acid, where mineral acids include hydrochloric acid, sulfuric acid, nitric acid, and potassium hydrogen sulfate.